EP4349839A3 - Inhibiteurs de kars dépendant d'akr1c3 tricycliques - Google Patents

Inhibiteurs de kars dépendant d'akr1c3 tricycliques Download PDF

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Publication number
EP4349839A3
EP4349839A3 EP23195635.0A EP23195635A EP4349839A3 EP 4349839 A3 EP4349839 A3 EP 4349839A3 EP 23195635 A EP23195635 A EP 23195635A EP 4349839 A3 EP4349839 A3 EP 4349839A3
Authority
EP
European Patent Office
Prior art keywords
kars
tricyclic
inhibitors
dependent
akr1c3
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP23195635.0A
Other languages
German (de)
English (en)
Other versions
EP4349839A2 (fr
Inventor
Chris ADAIR
Tracy Chen
Jian Ding
Christy FRYER
Yuko ISOME
Marie-Helene LARRAUFIE
Katsumasa Nakajima
Nik Savage
Ariel Sterling TWOMEY
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Priority to MA71308A priority Critical patent/MA71308A/fr
Publication of EP4349839A2 publication Critical patent/EP4349839A2/fr
Publication of EP4349839A3 publication Critical patent/EP4349839A3/fr
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4747—Quinolines; Isoquinolines spiro-condensed

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
EP23195635.0A 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques Pending EP4349839A3 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
MA71308A MA71308A (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962881619P 2019-08-01 2019-08-01
US202063009513P 2020-04-14 2020-04-14
US202063033932P 2020-06-03 2020-06-03
PCT/IB2020/057285 WO2021005586A1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques
EP20753456.1A EP4013500B1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques

Related Parent Applications (3)

Application Number Title Priority Date Filing Date
PCT/IB2020/057285 Previously-Filed-Application WO2021005586A1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques
EP20753456.1A Division EP4013500B1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques
EP20753456.1A Division-Into EP4013500B1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques

Publications (2)

Publication Number Publication Date
EP4349839A2 EP4349839A2 (fr) 2024-04-10
EP4349839A3 true EP4349839A3 (fr) 2024-10-02

Family

ID=71994691

Family Applications (2)

Application Number Title Priority Date Filing Date
EP20753456.1A Active EP4013500B1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques
EP23195635.0A Pending EP4349839A3 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP20753456.1A Active EP4013500B1 (fr) 2019-08-01 2020-07-31 Inhibiteurs de kars dépendant d'akr1c3 tricycliques

Country Status (37)

Country Link
US (3) US11970497B2 (fr)
EP (2) EP4013500B1 (fr)
JP (1) JP7008161B2 (fr)
KR (1) KR102735388B1 (fr)
CN (1) CN114206870B (fr)
AU (1) AU2020309846B2 (fr)
BR (1) BR112022001308A2 (fr)
CA (1) CA3139940A1 (fr)
CL (1) CL2022000201A1 (fr)
CO (1) CO2022000370A2 (fr)
CR (1) CR20220031A (fr)
CU (1) CU24698B1 (fr)
DK (1) DK4013500T3 (fr)
DO (1) DOP2022000010A (fr)
EC (1) ECSP22005621A (fr)
ES (1) ES2969591T3 (fr)
FI (1) FI4013500T3 (fr)
HR (1) HRP20231734T1 (fr)
HU (1) HUE064882T2 (fr)
IL (1) IL287792B2 (fr)
JO (1) JOP20220020B1 (fr)
LT (1) LT4013500T (fr)
MA (1) MA71308A (fr)
MX (1) MX2022000961A (fr)
MY (1) MY206964A (fr)
PE (1) PE20220343A1 (fr)
PH (1) PH12022550200A1 (fr)
PL (1) PL4013500T3 (fr)
PT (1) PT4013500T (fr)
PY (1) PY2039449A (fr)
RS (1) RS65068B1 (fr)
SA (1) SA522431533B1 (fr)
SI (1) SI4013500T1 (fr)
TW (1) TWI864063B (fr)
UY (1) UY38806A (fr)
WO (1) WO2021005586A1 (fr)
ZA (1) ZA202108632B (fr)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PH12021552839A1 (en) 2019-06-14 2022-10-03 Janssen Pharmaceutica Nv Substituted pyrazolo-pyridine amides and their use as glun2b receptor modulators
JP2022536773A (ja) 2019-06-14 2022-08-18 ヤンセン ファーマシューティカ エヌ．ベー． 置換ピラゾロピラジン及びｇｌｕｎ２ｂ受容体調節因子としてのそれらの使用
UY38806A (es) * 2019-08-01 2021-02-26 Novartis Ag Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos
TWI915409B (zh) 2020-09-02 2026-02-21 大陸商深圳艾欣達偉醫藥科技有限公司 一種akr1c3檢測方法、檢測akr1c3的診斷試劑盒及其用途
CN113135878A (zh) * 2021-04-09 2021-07-20 新沂市凯美斯特医药科技有限公司 一种以呋喃为原料合成3-氨基甲基四氢呋喃的方法
LT4334289T (lt) * 2021-05-07 2025-09-25 Organon R&D Finland Oy Nauji heterocikliniai junginiai, kompozicijos, jų gamybos būdai ir naudojimo būdai
CN115403579A (zh) * 2021-05-27 2022-11-29 上海拓界生物医药科技有限公司 一种新的螺环衍生物及其用途
WO2023174319A1 (fr) 2022-03-15 2023-09-21 深圳艾欣达伟医药科技有限公司 Méthode de traitement d'un patient atteint d'un cancer à mutation de brca
WO2023237080A1 (fr) 2022-06-10 2023-12-14 深圳艾欣达伟医药科技有限公司 Méthode de traitement d'un patient atteint d'un cancer avec promédicament activé par enzyme akr1c3
EP4561702A1 (fr) 2022-07-26 2025-06-04 Novartis AG Méthodes associées à l'administration d'un inhibiteur tricyclique de kars dépendant de akr1c3 de l'invention
KR20250040690A (ko) 2022-07-26 2025-03-24 노파르티스 아게 삼환식 akr1c3 의존성 kars 억제제의 제약 조성물 및 이의 제조 방법
WO2024023666A1 (fr) 2022-07-26 2024-02-01 Novartis Ag Formes cristallines d'un inhibiteur de kars dependant d'akr1c3
KR20260020475A (ko) 2023-06-06 2026-02-11 아센타위츠 파마슈티컬즈 리미티드 Akr1c3 효소 발현 수준과 kras 돌연변이의 상관관계 및 의학적 용도

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012076673A1 (fr) * 2010-12-10 2012-06-14 Boehringer Ingelheim International Gmbh Dérivés de 6 -amino- 2 - phénylamino- 1h-benzimidazole- 5 -carboxamide et leur utilisation en tant qu'inhibiteurs de la prostaglandine e2 synthase-1 microsomale
WO2020128768A1 (fr) * 2018-12-18 2020-06-25 Novartis Ag Dérivés n-(pyridin-2-ylsulfonyl)cyclopropanecarboxamide et leur utilisation dans le traitement d'une maladie médiée par cftr

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6476019B1 (en) * 1999-08-13 2002-11-05 Sepracor Inc. Spirocyclic ligands for sigma receptors, and libraries and methods of use thereof
WO2006023821A2 (fr) * 2004-08-20 2006-03-02 The Trustees Of Columbia University In The City Of New York Ligands pour aldocetoreductases
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
US9346803B2 (en) 2011-10-17 2016-05-24 Vanderbilt University Indomethacin analogs for the treatment of castrate-resistant prostate cancer
JP6704421B2 (ja) 2015-03-10 2020-06-03 アセンタウィッツ ファーマシューティカルズ リミテッド Ｄｎａアルキル化剤
US10167293B2 (en) * 2016-05-26 2019-01-01 Bayer Pharma Aktiengesellschaft [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanones
UY38806A (es) 2019-08-01 2021-02-26 Novartis Ag Compuestos inhibidores tricíclicos de kars dependientes de akr1c3, composiciones y sus usos

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012076673A1 (fr) * 2010-12-10 2012-06-14 Boehringer Ingelheim International Gmbh Dérivés de 6 -amino- 2 - phénylamino- 1h-benzimidazole- 5 -carboxamide et leur utilisation en tant qu'inhibiteurs de la prostaglandine e2 synthase-1 microsomale
WO2020128768A1 (fr) * 2018-12-18 2020-06-25 Novartis Ag Dérivés n-(pyridin-2-ylsulfonyl)cyclopropanecarboxamide et leur utilisation dans le traitement d'une maladie médiée par cftr

Also Published As

Publication number Publication date
JP7008161B2 (ja) 2022-01-25
EP4349839A2 (fr) 2024-04-10
KR20220025845A (ko) 2022-03-03
ES2969591T3 (es) 2024-05-21
IL287792A (en) 2022-01-01
EP4013500A1 (fr) 2022-06-22
PY2039449A (es) 2021-12-20
ZA202108632B (en) 2024-09-25
MA71308A (fr) 2025-04-30
CA3139940A1 (fr) 2021-01-14
MX2022000961A (es) 2022-02-14
PT4013500T (pt) 2024-01-11
PE20220343A1 (es) 2022-03-14
US20220315582A1 (en) 2022-10-06
TWI864063B (zh) 2024-12-01
FI4013500T3 (fi) 2024-01-19
US11970497B2 (en) 2024-04-30
JOP20220020A1 (ar) 2023-01-30
LT4013500T (lt) 2024-01-25
US20250179072A1 (en) 2025-06-05
CO2022000370A2 (es) 2022-01-28
BR112022001308A2 (pt) 2022-05-17
ECSP22005621A (es) 2022-02-25
CR20220031A (es) 2022-02-09
CL2022000201A1 (es) 2022-11-18
JP2021527113A (ja) 2021-10-11
CU20220005A7 (es) 2022-09-08
WO2021005586A1 (fr) 2021-01-14
HUE064882T2 (hu) 2024-04-28
PH12022550200A1 (en) 2022-11-14
HRP20231734T1 (hr) 2024-03-15
CU24698B1 (es) 2024-03-05
DK4013500T3 (da) 2024-01-02
IL287792B2 (en) 2025-04-01
PL4013500T3 (pl) 2024-03-25
SI4013500T1 (sl) 2024-02-29
EP4013500B1 (fr) 2023-10-25
RS65068B1 (sr) 2024-02-29
TW202120507A (zh) 2021-06-01
CN114206870A (zh) 2022-03-18
AU2020309846A1 (en) 2022-01-06
IL287792B1 (en) 2024-12-01
JOP20220020B1 (ar) 2024-12-22
MY206964A (en) 2025-01-22
SA522431533B1 (ar) 2024-04-16
UY38806A (es) 2021-02-26
CN114206870B (zh) 2024-09-03
KR102735388B1 (ko) 2024-11-29
DOP2022000010A (es) 2022-03-15
AU2020309846B2 (en) 2023-12-14
US20240262827A1 (en) 2024-08-08

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